Epitalon – also commonly referred to as Epithalamin and Epithalon – is a synthetic tetrapeptide, that is made up of 4 amino acids: Glutamic, Glycine, Aspartic, and Alanine. It has a molecular structure of C14H22N4O9 and a molecular weight of 390.35 grams per mole. It has a sequence of H-Ala-Glu-Asp-Gly-OH. Epitalon peptide is structurally the same as the naturally occurring “Epithalamin” peptide, a hormone the pineal gland creates. Epitalon is considered to be involved in metabolic functions; researchers suggest it may act to raise the hypothalamus’s sensitivity to its natural hormone and may affect the regulation of melatonin levels as seen in animal research models, thereby regulating the circadian rhythm. During research assessments, Epitalon peptide has presented curious results with regard to aspects of age-related physiological decline, and researchers suggest that it may support a certain amount of prolonged organ function. Prof. Vladimir Khavinson, a Russian scientist, first isolated Epitalon peptide and studied it rigorously for over 35 years. His findings make up the bulk of existing research on this peptide compound.
Epitalon peptide is typically handled in its lyophilized powder state. The powder may be diluted using a mild solution of acetic acid or water, typically distilled. The peptide is considered fairly stable for up to three months in its powder state and at room temperature. However, it requires a storage temperature of 4ºC once diluted. Research may be conducted with the compound anywhere between 2 to 21 days, so long as it remains stored at a stable temperature.
Scientists consider that telomeres, the structures located at the periphery of a chromosome, are responsible in part for the senescence of organs at a cellular level. Among the suggested impacts resulting from cell exposure to Epitalon peptide is an apparent elongation of telomere, potentially inhibiting, or halting age-associated cellular decline. Studies report that cell regeneration appears to have occurred following the cells’ exposure to the peptide. When carefully observed through a microscope, animal cells have presented that correction to some degree takes place at the level of the cell’s DNA, presenting potential hypotheses for results regarding the repair and regeneration of such cell structures. Researchers have suggested Epitalon’s potential to govern levels of melatonin and cortisol, as well as a potential to regulate hormones within the reproductive systems of female murine models.
Epitalon Peptide and Cell Aging
Researchers have suggested that the animal research models undergoing exposure to Epitalon peptide appear to function and survive longer than non-exposed control counterparts. Some models’ mortality rates have even been reduced by as much as 50%, which is nearly 1.5x longer than controls. The Epitalon-exposed rodents with prolonged lifespans reportedly did not suffer from any onset of Leukemia (any form); this was not true for the control group. The research team suggested Epitalon peptide may promote telomerase formation, the natural enzyme that aids in the cells’ reproduction of telomeres. Telomeres are considered to be protective elements of DNA, preventing the loss of genetic information. The function of telomeres results in the shortening of chromosomes, which takes place during cell division. Any time cells divide, telomeres shrink, which is why this process is closely associated with age-associated degenerative diseases, such as cognitive or cardiovascular diseases, and inevitably, cell death. With the intentional activation of telomerase, cells may potentially continue to proliferate, and even remain active past the normal life expectancy of typical cells. Epitalon, may therefore play a function in slowing the aging process of cells. Any form of impact that Epitalon peptide may exhibit requires the measurement of an endpoint – health span, aging biomarkers, or life span. Aging biomarkers must meet the following criteria:
- Supervise the underlying process of aging
- Must register effective in the laboratory animals under examination
- Endure repeated assessment with the test subject remaining unharmed
- Besides chronological age, it should also forecast lifespan
Prof. Vladimir Khavinson, in the course of over 30 years, conducted experiments on rodents and suggested telomere elongation results from their activation – both of which, he suggested, may potentially be caused by Epitalon peptide exposure. Studies have displayed researchers’ ability to manipulate a gene to mitigate age-related deterioration in rodents – albeit partially.
Depending on and determined by their DNA, cells play particular roles in the bodies within which they reside. As cells age, they release toxins around them, and they have a limited life span. The senior cells then go through the process of programmed cell death, apoptosis, in efforts to protect the organism. Rather than dying off and being organically disposed of within the organism, these old cells may sometimes stimulate diseases in tissues of other organs (liver, brains, kidney, heart, etc.). There is reasonable suspicion among researchers that aging may be due to these senior cells remaining present in vivo.
An experiment was performed on genetically engineered rodents that were manipulated to age more rapidly than seen in nature. The rodents’ telomeres were short and dysfunctional, and experienced a variety of age-related problems (shrunken brain, damaged intestines, impaired sense of smell, atrophied spleens, etc.). The hypothesis of the researchers was that, by promoting the telomerase activity – an enzyme that makes small DNA units called telomeres, which shut tight the chromosome tips, thus keeping the genes within from coming undone, aging may be mitigated within the rodent bodies. The rodents were exposed to Epitalon peptide, and after just one month, the rodents appeared to exhibit signs of cellular revitalization. Their telomerase levels were higher, and their telomeres appeared to have grown longer. As a result, the animals’ organs showed better function overall. The exposed rodents grew spleens, reinvigorated their olfactory senses, and the dormant stem cells of their brains grew in size and were reported to have formed new neurons. At the end of the experiment, the rodents exposed to Epitalon peptide displayed the physiological equivalence of human youth and thus a prolonged lifespan. Clinical trials of the peptide have suggested similar advantageous impacts reflected by the betterment of various organs’ conditions. The potential of Epitalon peptide may be exhibited through action on telomerase. Upon their multiplication, cells have a given amount of cycles they can perform. According to studies conducted by Prof Khavinson, cells exposed to Epitalon peptide produced a total of 44 passages, 10 additional divisions than control cells produced, on average.
Epitalon Peptide and Melatonin
Melatonin is produced and regulated by the pineal gland. Investigations in Epitalon peptide exposure in murine models displayed a notable reduction in melatonin concentration in the blood of the aging animals. The hormone melatonin is considered to play a crucial role in the nervous, endocrine, and immune system functioning. Supplementing melatonin levels is considered to induce a level of geroprotective impact. Such action, though, may possibly aggravate adverse impacts, such as neoplastic growth. Therefore, researchers are concerned with determining ways to stimulate the secretion of natural, endogenous melatonin. Epitalon has been suggested by researchers to possibly induce such a secretion, through research on the impact of the peptide in the neuroendocrine and immune systems. Studies are ongoing to further supplement these research hypotheses.
Epitalon Peptide and Cancer Research
Epitalon peptide may potentially slow the expansion of malignant tumors through its possible activating action on melatonin secretion, as discussed above, which may inhibit the advancement of metastasis. By examining the connection between the cancer cell proliferation and pineal gland, researchers have drawn conclusions as to how this happens, but as of yet no theories have been formalized. Research data presents a possible converse relationship between cancerous tumor growth (in various organs) and natural melatonin production.
Epitalon Peptide and Longevity, Antioxidant and Vision Research
Researchers suggest Epitalon peptide may stimulate the generation of telomerase, thus elongating and strengthening telomeres in the DNA strands. This may reduce apoptosis and prolongs cell lifespan, which in turn may have a downstream effect of reducing or delaying the onset of age-related diseases. When it comes to removing free radicals, the peptide has been suggested by research studies to provide potential antioxidant properties. It may remove oxygen-free radicals that contribute to cell destruction – considered the primary cause of degenerative diseases like Alzheimer’s. In rodent models of hereditary Retinitis Pigmentosa, Epitalon peptide was reported by researchers to exhibit workable integrity of their eyes’ retina. For models of pigmentary retinal degeneration, it appeared to enhance their overall vision.
- Anisimov VN, Khavinson VKh, Alimova IN, et al. Epithalon decelerates aging and suppresses the development of breast adenocarcinomas in transgenic her-2/neu mice. Bull Exp Biol Med, 2002.
- Kossoy G, Anisimov VN, Ben-Hur H, et al. Effect of the synthetic pineal peptide epitalon on spontaneous carcinogenesis in female C3H/He mice. In Vivo, 2006.
- Alimova IN, Bashurin DA, Popovich IG, et al. Effect of Epitalon and Vilon treatment on mammary carcinogenesis in transgenic erbB-2/NEU mice. Vopr Onkol, 2002.
- Khavinson VKh. Peptides and Ageing. Neuro Endocrinol Lett, 2002.
- Kozina LS, Arutjunyan AV, Khavinson VKh. Antioxidant properties of geroprotective peptides of the pineal gland. Arch Gerontol Geriatr, 2007.
- Khavinson VKh, Bondarev IE, Butyugov AA. Epithalon peptide induces telomerase activity and telomere elongation in human somatic cells. Bull Exp Biol Med, 2003.
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